Dabrafenib (GSK2118436)是一种突变型BRAFV600特异性抑制剂,IC50为0.8 nM,作用于B-Raf(wt)和c-Raf效果低4和6倍。
Dabrafenib is a specific inhibitor of BRAF V600 mutants with IC50 values of 0.5nM, 0.6nM and 1.9nM against V600E, V600K and V600D, respectively.
30% PEG400+0.5% Tween80+5% Propylene glycol
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.
分子式 C23H20F3N5O2S2 |
分子量 519.56 |
CAS号 1195765-45-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 30 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02700763 | Melanoma | Other: [18F]dabrafenib molecular imaging | University Medical Center Groningen | Phase 1 | 2016-10-01 | 2016-09-13 |
NCT01972347 | Melanoma | Drug: Dabrafenib|Drug: Trametinib | Melanoma Institute Australia | Phase 2 | 2014-10-01 | 2017-03-21 |
NCT01682213 | Melanoma | Drug: Dabrafenib | Memorial Sloan Kettering Cancer Center|National Comprehensive Cancer Network|Novartis | Phase 2 | 2012-09-01 | 2016-06-07 |
NCT02052193 | Metastatic Melanoma (Carrying BRAF V600 Mutation) | Drug: Dabrafenib|Drug: Vemurafenib | University Hospital Tuebingen | Phase 2 | 2014-01-01 | 2015-07-17 |
NCT02231775 | Melanoma | Drug: Dabrafenib|Drug: Trametinib|Procedure: Surgery | M.D. Anderson Cancer Center|Novartis Pharmaceuticals | Phase 2 | 2014-10-01 | 2017-02-10 |
NCT01726738 | Stage III Melanoma|Stage IV Melanoma|Unresectable Melanoma|BRAF Mutant Melanoma | Drug: BRAF inhibitor dabrafenib and MEK inhibitor trametinib | UNC Lineberger Comprehensive Cancer Center|GlaxoSmithKline | Phase 2 | 2012-10-01 | 2017-03-02 |
NCT01721603 | BRAFV600E Melanoma Patients | Drug: Dabrafenib|Procedure: Gamma Knife Radiosurgery | University of California, San Francisco|GlaxoSmithKline | Phase 2 | 2013-04-01 | 2016-10-28 |
NCT02367859 | Ameloblastoma|BRAF Gene Mutation | Drug: Dabrafenib|Other: Laboratory Biomarker Analysis | Stanford University|National Cancer Institute (NCI) | Phase 2 | 2017-04-01 | 2017-03-01 |
NCT02974803 | Melanoma|Brain Metastases | Drug: Dabrafenib|Drug: Trametinib | Canadian Cancer Trials Group|Novartis | Phase 2 | 2016-11-01 | 2017-03-08 |
NCT02447939 | Melanoma | Drug: Dabrafenib|Drug: Trametinib | GlaxoSmithKline | Phase 1 | 2017-05-01 | 2017-01-25 |
NCT01947023 | BRAF V600E Mutation Present|BRAF V600K Mutation Present|Metastatic Malignant Neoplasm in the Thyroid Gland|Recurrent Thyroid Gland Carcinoma|Unresectable Thyroid Gland Carcinoma | Drug: Dabrafenib|Other: Laboratory Biomarker Analysis|Drug: Lapatinib Ditosylate|Other: Pharmacological Study | National Cancer Institute (NCI) | Phase 1 | 2013-08-01 | 2016-12-21 |
NCT01907802 | BRAF Gene Mutation|Hepatic Complication|Renal Failure|Solid Neoplasm | Drug: Dabrafenib|Other: Laboratory Biomarker Analysis|Other: Pharmacogenomic Study|Other: Pharmacological Study | National Cancer Institute (NCI)|Glaxosmithkline Biologicals S.A. | Phase 1 | 2013-08-01 | 2017-01-31 |
NCT01978236 | Melanoma and Brain Metastases | Drug: Dabrafenib 150 mg|Drug: Trametinib 2.0 mg | GlaxoSmithKline | Phase 2 | 2014-04-01 | 2016-12-02 |
NCT02684058 | Anaplastic Astrocytoma|Glioblastoma|Giant Cell Glioblastoma|Gliosarcoma|Anaplastic Oligodendroglioma|Anaplastic Oligoastrocytoma|Anaplastic Ependymoma|Choroid Plexus Carcinoma|Anaplastic Ganglioglioma|Pineal Parenchymal Tumor|Pineoblastoma|Medulloblastoma|PNET|Rhabdoid Tumor|Perineurioma|MPNST|Malignant Meningloma|Anaplastic Hemangiopericytoma | Drug: dabrafenib | Novartis Pharmaceuticals|Novartis | Phase 2 | 2017-07-17 | 2017-02-13 |
NCT02672358 | Non-Small-Cell Lung Cancer | Drug: Dabrafenib|Drug: Trametinib | Novartis Pharmaceuticals|Novartis | Phase 2 | 2017-10-01 | 2017-01-03 |
NCT02296996 | Malignant Melanoma | Drug: Dabrafenib + Trametinib | Universitair Ziekenhuis Brussel | Phase 2 | 2014-10-01 | 2016-09-08 |
NCT02034110 | Cancer | Drug: Dabrafenib|Drug: Trametinib | GlaxoSmithKline | Phase 2 | 2014-03-01 | 2017-02-23 |
NCT02200562 | Stage III or IV Melanoma | Drug: ipilimumab and dabrafenib | University of Utah | Phase 1 | 2014-12-01 | 2017-02-27 |
NCT01767454 | Solid Tumours | Drug: Dabrafenib|Drug: Trametinib|Drug: Ipilimumab | GlaxoSmithKline | Phase 1 | 2013-02-01 | 2017-01-23 |
NCT01677741 | Neoplasms, Brain | Drug: Dabrafenib | GlaxoSmithKline | Phase 1 | 2013-02-01 | 2017-03-04 |
NCT01584648 | Melanoma | Drug: dabrafenib|Drug: dabrafenib plus trametinib placebo|Drug: Trametinib | GlaxoSmithKline | Phase 3 | 2012-05-01 | 2017-01-10 |
NCT02083354 | Cancer | Drug: Dabrafenib|Drug: Trametinib | GlaxoSmithKline | Phase 2 | 2014-03-01 | 2017-03-23 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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